Table 3.

BET degraders (PROTACs) with their components and mechanism of action

CompoundBET inhibitor componentSmall-molecule componentE3 ubiquitin ligase complexReference
ARV-771JQ1VHL ligandVon Hippel–Lindau-containing complex(111)
ARV-825OTX015ThalidomideCereblon E3 ubiquitin ligase complex(107)
AT1JQ1VHL ligandVon Hippel–Lindau-containing complex(136)
BETd-246RX-37ThalidomideCereblon E3 ubiquitin ligase complex(113)
BETd-260/ZBC260HJB97/Beti-211LenalidomideCereblon E3 ubiquitin ligase complex(113, 137)
dBET1JQ1ThalidomideCereblon E3 ubiquitin ligase complex(138)
dBET6JQ1ThalidomideCereblon E3 ubiquitin ligase complex(4)
MZ1JQ1VHL ligandVon Hippel–Lindau-containing complex(139)